Assay Detail
Binding
CHEMBL871977
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Displacement of [3H]-Rolipram from mouse brain homogenates
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Brain |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Expert |
Publication
Synthesis and in vitro profile of a novel series of catechol benzimidazoles. The discovery of potent, selective phosphodiesterase type IV inhibitors with greatly attenuated affinity for the [3H]rolipram binding site
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.97 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 8.40 |
| CHEMBL58915 | — | — | 1 | 7.50 |
| CHEMBL294883 | — | — | 1 | 7.11 |
| CHEMBL59269 | — | — | 1 | 6.89 |
| CHEMBL291537 | — | — | 1 | 6.66 |
| CHEMBL60073 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63 | ROLIPRAM | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL58915 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL294883 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL59269 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL291537 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL60073 | — | IC50 | = | 5910.0 | nM | 5.23 |